GW2974

GW2974 is a potent, reversible, and orally active dual inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2/ErbB2) tyrosine kinases. Developed by GSK (formerly Glaxo Wellcome), GW2974 is structurally related to lapatinib. It was investigated preclinically for its potential in treating various cancers, including breast cancer and glioblastoma multiforme, but was not progressed to clinical trials due to unfavorable pharmacokinetic properties. In preclinical studies, GW2974 demonstrated significant anti-proliferative and anti-tumor activity by blocking EGFR and HER2 phosphorylation and downstream signaling pathways.

Other names

4-N-(1-benzylindazol-5-yl)-6-N,6-N-dimethylpyrido[3,4-d]pyrimidine-4,6-diamineN4-(1-benzyl-1H-indazol-5-yl)-N6,N6-dimethyl-pyrido[3,4-d]pyrimidine-4,6-diamineN6,N6-dimethyl-N4-[1-(phenylmethyl)-5-indazolyl]pyrido[3,4-d]pyrimidine-4,6-diamine